Sigma Receptor
Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body. The endogenous ligand for these sites has not been identified, but steroid hormones (particularly progesterone), sphingolipid-derived amines and N,N-dimethyltryptamine can bind with fairly high affinity.
The sigma-1 receptor (σ1R) is an endoplasmic reticulum (ER)-resident chaperone protein that acts like an inter-organelle signaling modulator. It participates in many biological processes including nociception, cancer, stroke, memory, drug addiction, cardiac activity, and Alzheimer’s disease. The sigma-2 (σ2R) receptor is overexpressed in various human tumors. It has been validated as a biomarker for proliferating tumors.
Sigma Receptor Isoform Specific Products
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Sigma Receptor Inhibitors
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Sigma Receptor Agonists
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Sigma Receptor Antagonists
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Sigma Receptor Activators
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Sigma Receptor Modulators
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Sigma Receptor Control
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Sigma Receptor Ligands
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Sigma Receptor Related Products (196)
Related Products (196)
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Sigma Receptor Isoform Comparison
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SUN-1334H free base
0 ImagesCat. No.: HY-164010CAS No.: 607737-00-8SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.
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SW43
0 ImagesCat. No.: HY-122224CAS No.: 1590379-85-3SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA (89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis.
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(Rac)-E1R
0 Images(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.
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CM304 free base
0 ImagesCat. No.: HY-129485ACAS No.: 1350296-21-7Synonyms: FTC-146CM304 free base (FTC-146) is a potent S1R antagonist. CM304 free base enhances the antinociceptive effects of the cannabinoid receptor agonists. CM304 free base inhibits convulsions in rats.
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BGC-201259
0 ImagesCat. No.: HY-107047CAS No.: 444667-97-4Synonyms: RS-1259BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease.
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(2R,3S)-E1R
0 Images(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
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SV119
0 ImagesCat. No.: HY-177345CAS No.: 913815-82-4SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer.
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SIGMAR1 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS12908SIGMAR1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIGMAR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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PW507
0 ImagesCat. No.: HY-161873CAS No.: 2573850-59-4PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN).
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CM764
0 ImagesCat. No.: HY-117420CAS No.: 1350296-29-5CM764 is an activator for sigma receptor with Ki of 86.6 and 3.5 nM for sigma-1 receptor and sigma-2 receptor. CM764 increases cytoplasmic calcium, NAD+/NADH, and ATP levels, and decreases the concentration of ROS.
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SAS-1121
0 ImagesCat. No.: HY-120008CAS No.: 2095551-67-8SAS-1121 is a subtype-selective sigma 2 receptor/PGRMC1 ligand with a Ki of 16.2 nM. SAS-1121 is 574-fold selective for the signma 2 receptor over the sigma 1 receptor. SAS-1121 is a tertiary amine. SAS-1121 can be studied in neurology-related research.
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Sigma-1 receptor antagonist 7
0 ImagesCat. No.: HY-187185CAS No.: 3050643-44-9Sigma-1 receptor antagonist 7 is a selective sigma-1 receptor antagonist capable of crossing the blood-brain barrier, with an IC50 of 12.7 nM against guinea pig σ1R. Sigma-1 receptor antagonist 7 binds to σ1R, and its binding affinity decreases in the presence of Phenytoin (HY-B0448). Sigma-1 receptor antagonist 7 alleviates mechanical and thermal hyperalgesia induced by acute inflammation in rats. Sigma-1 receptor antagonist 7 can be used for research related to hyperalgesia.
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AB21 oxalate
0 ImagesCat. No.: HY-149854AAB21 oxalate is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity.
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(2R,3R)-E1R
0 Images(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
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Opipramol dihydrochloride
0 ImagesCat. No.: HY-118901ACAS No.: 909-39-7Synonyms: Ensidon dihydrochloride; G-33040 dihydrochlorideOpipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).
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CB-64D
0 ImagesCat. No.: HY-120360CAS No.: 157752-20-0CB-64D is the agonist for sigma receptor 2 and sigma receptor 1 with Ki of 16.5 and 3063 nM. CB-64D induces apoptosis in cancer cell SK-N-SH.
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Caprospinol
0 ImagesCaprospinol (SP-233) is a steroid compound candidate based on the structure of 22R-hydroxycholesterol. It has multiple mechanisms of neuroprotection, including binding to β-amyloid protein (Aβ(42)), interacting with the mitochondrial respiratory chain, clearing Aβ(42) monomers, and acting as a σ-1 receptor ligand. It can cross the blood-brain barrier in vivo and restore cognitive impairment, and has the potential to inhibit Alzheimer's disease.
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E-5842 citrate
0 ImagesCat. No.: HY-106153BCAS No.: 220120-14-9E-5842 citrate is a σ receptor ligand (Ki: 4 nM for σ1 receptor). E-5842 citrate increases levels of Fos in the medial prefrontal cortex and the nucleus accumbens, without affecting the levels of the protein in the striatum. E-5842 citrate can be used in the research of psychiatric disorders.
